Taste-masked oral pharmaceutical composition
Inventors
DANDL, KLAUS • HAACK, DETLEV • Becker, Karin • Zimmer, Andreas • Lang, Claudia • SALAR BEHZADI, Sharareh
Assignees
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Publication Number
US-10314801-B2
Publication Date
2019-06-11
Expiration Date
Abstract
The invention provides coated particles with a taste-masked drug substance. The particles comprise a core with the agglomerated active ingredient and a coating comprising a triglyceride and a surfactant. The particles exhibit rapid drug release and a stable release profile. Moreover, the invention provides a hot-melt coating method for manufacturing such particles, and pharmaceutical compositions comprising the particles. The method allows the coating of core particles at moderate temperatures, thereby preventing the degradation of the thermolabile active ingredient.
Core Innovation
The invention relates to an immediate release particle comprising a core and a coating, wherein the core consists of an agglomerated granule or pellet having a diameter in the range from about 100 μm to about 1000 μm and consists of an agglomerated active ingredient. The particle further includes a coating that consists of a triglyceride which is solid at room temperature and a polysorbate surfactant.
The disclosed approach uses a triglyceride/surfactant coating system to achieve taste-masking while maintaining immediate release and rapid dissolution. The coating is described as being applied as a hot-melt at moderate product temperatures, so that the coating components can be introduced without changing the release profile during storage.
The document describes pharmaceutical compositions in dosage forms that include these coated particles, such as dispersible/effervescent/direct-to-mouth granules and orally disintegrating tablets. Examples are described for taste-masked immediate release systems using active ingredients such as ibuprofen sodium, paracetamol, calcium acetate, and caffeine, where rapid dissolution and maintained taste-masking are reported.
Claims Coverage
The partial content provides two independent claims. Across these claims, the inventive coverage centers on an immediate release coated particle with an agglomerated active-ingredient core of about 100 μm to about 1000 μm diameter and a coating composed of a room-temperature-solid triglyceride plus a polysorbate surfactant, including an obtainable coating method defined by providing a molten triglyceride-based coating composition and coating the core particle.
Immediate release particle with agglomerated core and triglyceride/polysorbate coating
An immediate release particle comprising a core and a coating, wherein the core consists of an agglomerated granule or pellet having a diameter in the range from about 100 μm to about 1000 μm, which core consists of an agglomerated active ingredient, and wherein the coating consists of a triglyceride which is solid at room temperature and a polysorbate surfactant.
Coated particle obtainable by molten triglyceride/polysorbate coating steps
A particle comprising a core and a coating, wherein the core consists of an agglomerated granule or pellet having a diameter in the range from about 100 μm to about 1000 μm, which consists of an agglomerated active ingredient, and wherein the coating consists of a triglyceride which is solid at room temperature and a polysorbate surfactant, said particle being obtainable by a method comprising providing a core particle consisting of an agglomerated active ingredient, providing a coating composition consisting of a molten triglyceride which is a solid at room temperature and a polysorbate surfactant, and coating the core particle with the coating composition.
Both independent claims define a coated immediate-release particle with an agglomerated active-ingredient core of about 100 μm to about 1000 μm diameter and a coating containing a triglyceride solid at room temperature plus a polysorbate surfactant, with the second independent claim additionally requiring that the particle is obtainable by applying a molten triglyceride/polysorbate coating composition to the core particle.
Stated Advantages
Rapid dissolution is achieved while maintaining taste-masking.
Dissolution performance is maintained without changing the release profile during storage.
Storage stability is reported for dissolution performance and taste-masking.
Documented Applications
Taste-masked immediate release oral pharmaceutical compositions and dosage forms including dispersible/effervescent/direct-to-mouth granules and orally disintegrating tablets.
Taste-masked immediate release example systems for ibuprofen/ibuprofen sodium, paracetamol/acetaminophen, calcium acetate, and caffeine.
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